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BRD4 (BD1)

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (1) AMPK (1) Apoptosis (11) Bcl-2 Family (1) c-Fms (1) c-Myc (5) Caspase (1) CDK (3) Discoidin Domain Receptor (1) DNA/RNA Synthesis (1) E3 Ligase Ligand-Linker Conjugates (1) Epigenetic Reader Domain (103) Fluorescent Dye (1) Histone Acetyltransferase (3) HIV (2) Interleukin Related (3) Ligands for Target Protein for PROTAC (1) Molecular Glues (1) NF-κB (2) p38 MAPK (1) PAK (1) Phosphatase (1) PI3K (4) Polo-like Kinase (PLK) (1) PROTACs (21) Reactive Oxygen Species (ROS) (1) Reference Standards (2) SARS-CoV (1) STAT (1) TNF Receptor (2)
By Research Areas:	Cancer (87) Cardiovascular Disease (2) Infection (4) Inflammation/Immunology (28) Metabolic Disease (1) Neurological Disease (1)
Click Chemistry:	PROTAC Synthesis (2) Azide (1)

105

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Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-107425

MZ 1 20+ Cited Publications	PROTACs Epigenetic Reader Domain	Cancer
MZ 1 is a PROTAC connected by ligands for von Hippel-Lindau and *BRD4. MZ 1 potently and rapidly induces reversible, long-lasting, and selective removal of BRD4* over BRD2 and BRD3. K_ds of 382/120, 119/115, and 307/228 nM for **BRD4 BD1/2*, BRD3 BD1/2, and BRD2 BD1*/2, respectively ^[1].

HY-16954

ARV-825 Maximum Cited Publications 35 Publications Verification	PROTACs Epigenetic Reader Domain	Cancer
ARV-825 is a PROTAC connected by ligands for Cereblon and *BRD4. ARV-825 binds to BD1* and BD2 of BRD4 with K_ds of 90 and 28 nM, respectively.

HY-12863

Pelabresib CPI-0610	Epigenetic Reader Domain	Cancer
Pelabresib (CPI-0610) is a potent, selective, orally active and cell-active BET inhibitor. Pelabresib inhibits *BRD4-BD1* with an IC₅₀ of 39 nM, and with an EC₅₀ value of 0.18 μM for MYC ^[1].

HY-136570

GSK778 1 Publications Verification iBET-BD1	Epigenetic Reader Domain Apoptosis	Inflammation/Immunology Cancer
GSK778 (iBET-BD1), a chemical probe, is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC₅₀s of 75 nM (BRD2 *BD1), 41 nM (BRD3* *BD1), 41 nM (BRD4* *BD1), and 143 nM (BRDT BD1), respectively. GSK778 phenocopies the effects of pan-BET* inhibitors in cancer models ^[1].

HY-111139

MS417 4 Publications Verification GTPL7512	Epigenetic Reader Domain HIV	Infection Inflammation/Immunology
MS417 is a selective BET-specific *BRD4* inhibitor, binds to BRD4-BD1 and BRD4-BD2 with IC₅₀s of 30, 46 nM and K_ds of 36.1, 25.4 nM, respectively, with weak selectivity at CBP BRD (IC₅₀, 32.7 μM).

HY-112609

QCA570	PROTACs Epigenetic Reader Domain	Cancer
QCA570 is a PROTAC connected by ligands for Cereblon and BET, with an IC₅₀ of 10 nM for **BRD4 BD1** Protein.

HY-114204

GSK8814 1 Publications Verification	Epigenetic Reader Domain	Cancer
GSK8814 is a potent and selective ATAD2 bromodomain chemical probe and inhibitor (IC₅₀ = 0.059 μM), with a binding constant pK_d = 8.1 and a pK_i = 8.9 in BROMOscan. GSK8814 binds to ATAD2 and BRD4 BD1 with *pIC₅₀s of 7.3 and 4.6, respectively. GSK8814 shows 500-fold selectivity for ATAD2 over BRD4* BD1. GSK8814 can be researched for cancer associated with ATAD2 bromodomain ^[1] .**

HY-129937A

GNE-987 1 Publications Verification	PROTACs Epigenetic Reader Domain	Cancer
GNE-987 is a VHL-dependent BRD4 PROTAC degrader. GNE-987 exhibits picomolar cell *BRD4* degradation activity (DC₅₀=0.03 nM for EOL-1 AML cell line). GNE-987 binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low nanomolar affinities (IC₅₀=4.7 and 4.4 nM, respectively). GNE-987 can be used for the research of cancer ^[1].

HY-100482

CPI-637 10+ Cited Publications	Epigenetic Reader Domain Histone Acetyltransferase	Cancer
CPI-637 is a selective and potent CBP/EP300 bromodomain inhibitor with IC₅₀ values of 0.03 μM, 0.051 μM and 11.0 μM for CBP, EP300 and **BRD4 BD-1, respectively, and an EC₅₀ of 0.3 μM for CBP** ^[1].

HY-111422

PLX51107 3 Publications Verification	Epigenetic Reader Domain	Cancer
PLX51107 is a potent and selective BET inhibitor, with K_ds of 1.6, 2.1, 1.7, and 5 nM for BD1 and 5.9, 6.2, 6.1, and 120 nM for BD2 of BRD2, BRD3, BRD4, and BRDT, respectively; PLX51107 also interacts with the bromodomains of CBP and EP300 (K_d, in the 100 nM range).

HY-151594

iBRD4-BD1	Epigenetic Reader Domain	Inflammation/Immunology Cancer
iBRD4-BD1 is selective BRD4 bromodomain inhibitor. iBRD4-BD1 has inhibition activity for BRD4 bromodomain with an IC₅₀ value of 12 nM. iBRD4-BD1 can be used for the research of inflammation and oncology ^[1].

HY-136857

BRD4 degrader-3	Epigenetic Reader Domain	Cancer
BRD4 degrader-3 is a potent bromodomain BRD4 degrader extracted from patent WO2020055976A1, example 1a, has IC₅₀s of 15.5 and 12.3 nM for BRD4-BD1 and BRD4-BD2, respectively ^[1]. PROTAC BRD4 Degrader-7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-145550

Amredobresib BI894999	Epigenetic Reader Domain	Cancer
Amredobresib (BI894999) is an orally active BET inhibitor. Amredobresib inhibits the binding of *BRD4-BD1* and *BRD4-BD2* bromodomains to acetylated histones with IC₅₀ values of 5 nM and 41 nM, respectively. Amredobresib exhibits anticancer activity against acute myeloid leukemia (AML) and NUT cancer ^[1] ^[4] .

HY-162514

BBC0403	Epigenetic Reader Domain	Inflammation/Immunology
BBC0403 is a selective *BRD2* inhibitor with K_ds of 7.64 μM and 41.37 μM for BRD2 (BD2) and **BRD2 (BD1)*, respectively. BBC0403 exhibitS higher binding specificity for BRD2 compared to BRD3 and BRD4*. BBC0403 has the potential for osteoarthritis (OA) research ^[1].

HY-120000

MS402 2 Publications Verification	Epigenetic Reader Domain	Inflammation/Immunology Cancer
MS402 is a *BD1*-selective BET BrD inhibitor with K_is of 77 nM, 718 nM, 110 nM, 200 nM, 83 nM, and 240 nM for *BRD4(BD1), BRD4(BD2), BRD3(BD1), BRD3(BD2), BRD2(BD1)* and *BRD2(BD2)*, respectively. MS402 blocks Th17 cell differentiation and ameliorates colitis in mice ^[1].

HY-133131

PROTAC BRD4 Degrader-1	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-1 is a PROTAC connected by ligands for Cereblon and *BRD4* with an IC₅₀ of 41.8 nM against BRD4 BD1. PROTAC BRD4 Degrader-1 can effectively degrade BRD4 protein and suppress c-Myc expression ^[1].

HY-112429

HJB97 2 Publications Verification	Ligands for Target Protein for PROTAC Epigenetic Reader Domain	Cancer
HJB97 is a high-affinity BET inhibitor with K_i values of 0.9 nM (BRD2 *BD1), 0.27 nM (BRD2* BD2), 0.18 nM (BRD3 *BD1), 0.21 nM (BRD3* BD2), 0.5 nM (BRD4 *BD1), and 1.0 nM (BRD4* BD2) ^[1]. HJB97 can serve as a ligand for target protein (Ligands for Target Protein for PROTAC) for the development of PROTAC BET degraders with antitumor activity ^[1]. HJB97 can be used for the synthesis of BETd-260 (HY-101519).

HY-133136

PROTAC BRD4 Degrader-2	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-2 is a PROTAC connected by ligands for Cereblon and *BRD4* with an IC₅₀ of 14.2 nM against **BRD4 BD1** ^[1].

HY-125232

MS645 1 Publications Verification	Epigenetic Reader Domain	Cancer
MS645 is a bivalent BET bromodomains (BrD) inhibitor with a K_i of 18.4 nM for BRD4-BD1/BD2. MS645 spatially constrains bivalent inhibition of BRD4 BrDs resulting in a sustained repression of BRD4 transcriptional activity in solid-tumor cells ^[1].

HY-138555

PROTAC BRD4 Degrader-8	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-8 is a PROTAC connected by ligands for von Hippel-Lindau and *BRD4, with IC₅₀s of 1.1 nM and 1.4 nM for *BRD4 BD1 and BD2*, respectively. PROTAC BRD4* Degrader-8 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells ^[1].

HY-151593

dBRD4-BD1	PROTACs Epigenetic Reader Domain	Cancer
dBRD4-BD1 is a selective and durable *BRD4* degrader with an DC₅₀ value of 280 nM (D_max=77%). dBRD4-BD1 upregulates BRD2/3 protein level and shows low cytotoxicity than iBRD4-BD1 ^[1].

HY-112610

CF53	Epigenetic Reader Domain Histone Acetyltransferase	Cancer
CF53 is a highly potent, selective and orally active inhibitor of BET protein, with a K_i of <1 nM, K_d of 2.2 nM and an IC₅₀ of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, very selective over non-BET bromodomain-containing proteins. CF53 shows potent anti-tumor activity both in vitro and in vivo ^[1].

HY-156820

HLDA-221	Epigenetic Reader Domain	Cancer
HLDA-221 is a non-covalent regulated induced proximity targeting chimeras (RIPTAC). The binding of HLDA-221 to *BRD4-BD1* is significantly increased after pre-incubation with FKBP. HLDA-221 can be used in cancer research ^[1].

HY-19760

I-BET282	Epigenetic Reader Domain	Inflammation/Immunology
I-BET282 is a pan-inhibitor of all eight BET bromodomains, and selectivity over other representative bromodomain-containing proteins. I-BET282 shows pIC₅₀s ranging 6.4-7.7 for BRD2 (BD1/BD2), BRD2 (BD1/BD), BRD3 (BD1/BD), and BRD4 (BD1/BD) .

HY-126428

ZL0580 1 Publications Verification	HIV Epigenetic Reader Domain	Infection Inflammation/Immunology
ZL0580, a structurally close analog of ZL0590, induces epigenetic suppression of HIV via selectively binding to BD1 domain of *BRD4*. ZL0580 induces HIV suppression by inhibiting Tat transactivation and transcription elongation as well as by inducing repressive chromatin structure at the HIV promoter ^[1] .

HY-178041

BRD4-BD1/2-IN-3	Epigenetic Reader Domain Interleukin Related c-Fms NF-κB TNF Receptor	Inflammation/Immunology
BRD4-BD1/2-IN-3 (Compound B6) is a selective BRD4 BD2 inhibitor with an IC₅₀ of 0.41  nM for BRD4 BD2 over BRD4 BD1. BRD4-BD1/2-IN-3 significantly inhibits the LPS (HY-D1056)-induced expression of IL-6. BRD4-BD1/2-IN-3 shows anti-inflammatory activities by modulating the TNF and NF-κB signaling pathway. BRD4-BD1/2-IN-3 can be used for inflammatory diseases research ^[1].

HY-117491

BRD4 Inhibitor-10	Epigenetic Reader Domain	Cancer
BRD4 Inhibitor-10 (Compound II-25) is a potent *BRD4-BD1* inhibitor with an IC₅₀ of 8 nM. BRD4 Inhibitor-10 can be used to study diseases caused by abnormal or excessive cell proliferation, such as cancer ^[1].

HY-146208

BRD4 Inhibitor-20 1 Publications Verification	Epigenetic Reader Domain	Cancer
BRD4 Inhibitor-20 is a potent orally active bromodomain protein 4 (BRD4) inhibitor. BRD4 Inhibitor-20 has inhibitory activity for BRD4 (BD1) and BRD4 (BD2) with IC₅₀ values of 19 nM and 28 nM, respectively. BRD4 Inhibitor-20 also has anti-proliferation activities in cancer cell lines. BRD4 Inhibitor-20 can be used for the research of kinds of cancer, such as colon cancer ^[1].

HY-145310

ZL0590	Epigenetic Reader Domain	Inflammation/Immunology
ZL0590 is a potent, orally active **BRD4 BD1**-selective inhibitor with an IC₅₀ of 90 nM for human BRD4 BD1. ZL0590 exhibits significant anti-inflammatory activities. ZL0590 can reduce mucosal inflammation in animal models of inflammatory bowel disease and restores tissue architecture. ZL0590 can be used in research on inflammatory diseases such as inflammatory bowel disease ^[1] .

HY-130622

LT052 1 Publications Verification	Epigenetic Reader Domain	Inflammation/Immunology
LT052 is a highly selective BET BD1 inhibitor with an IC₅₀ of 87.7 nM. LT052 exhibits nanomolar BRD4 BD1 potency and 138-fold selectivity over BRD4 BD2 (IC₅₀=12.130 μM). LT052 has anti-inflammatory?activity and can be used for acute gout arthritis research ^[1].

HY-112150

ZL0454 2 Publications Verification	Epigenetic Reader Domain	Inflammation/Immunology
ZL0454 is a potent and selective Bromodomain-containing protein 4 (BRD4) inhibitor with an IC₅₀ of 49 and 32 nM for BD1 and BD2.

HY-124596

CD161	Epigenetic Reader Domain	Cancer
CD161 is a potent, selective and orally bioavailable bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC₅₀s of 28.2 nM and 7.2 nM for BRD4 BD1 and BRD4 BD2, respectively. CD161 has good anticancer activity ^[1].

HY-163729

I-BET787	Epigenetic Reader Domain	Inflammation/Immunology Cancer
I-BET787 is a orally active BET bromine domain inhibitor with pIC₅₀s of 7.1 and 5.9 for BRD4 BD1 and BRD4 BD2, respectively. I-BET787 has anti-inflammatory activity in mice ^[1].

HY-133138

Pomalidomide-PEG1-azide	E3 Ligase Ligand-Linker Conjugates	Cancer
Pomalidomide-PEG1-azide is an E3 ligase lgand-linker conjugate. Pomalidomide-PEG1-azide incorporates the Pomalidomide based cereblon ligand and a linker. Pomalidomide-PEG1-azide can be used to synthesis PROTAC BRD4 Degrader-1 (HY-133131) ^[1]. PROTAC BRD4 Degrader-1 is a PROTAC connected by ligands for Cereblon and BRD4 with an IC₅₀ of 41.8 nM against **BRD4 BD1*. PROTAC BRD4* Degrader-1 can effectively degrade BRD4 protein and suppress c-Myc expression.

HY-153894

SRX3177	CDK Epigenetic Reader Domain PI3K NF-κB SARS-CoV	Infection Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
SRX3177 is a triple inhibitor of *CDK4/6, PI3K, and BRD4, with IC₅₀s of <2.5 nM (CDK4), 3.3 nM (CDK6), 33 nM (BRD4* BD1), 89 nM (BRD4 BD2), 79 nM (PI3Kα), 83 nM (PI3Kδ), 3.18 μM (PI3Kγ) , respectively. SRX3177 blocks the interaction between the SARS-CoV-2 E protein and the *BRD2/4* BD1 domain, restores E protein-attenuated NF-κB activity. SRX3177 exerts broad cytotoxic activity against cancer cells. SRX3177 can be used for the study of anti-SARS-CoV-2 and cancer ^[1] .

HY-138563

GSK973	Epigenetic Reader Domain	Cancer
GSK973, a chemical probe, is a highly selective, orally bioavailable inhibitor of the BD2s (second bromodomains) of the BET family, with a pIC₅₀ of 7.8 and a pK_d of 8.7 for BRD4 BD2. GSK973 displays a 1600-fold selectivity for BRD4 BD2 over BRD4 BD1. GSK973 shows good potency against BRD2 BD2, BRD3 BD2, and BRDT BD2 (pIC₅₀=7.4~7.8; pK_d=8.3~8.5) ^[1].

HY-142520

I-BET567	Epigenetic Reader Domain	Inflammation/Immunology Cancer
I-BET567 is a potent and orally active inhibitor of pan-BET candidate with pIC₅₀s of 6.9 and 7.2 for BRD4 BD1 and BD2, respectively. I-BET567 has been demonstrated efficacy in mouse models of oncology and inflammation ^[1].

HY-160558

PLK1/BRD4-IN-3	Epigenetic Reader Domain Polo-like Kinase (PLK)	Cancer
PLK1/BRD4-IN-3 (Compound 21) is a selective dual inhibitor for bromodomain 4 (BRD4) and polo-like kinase 1 (PLK1). PLK1/BRD4-IN-3 inhibits BRD4-BD1, PLK1 and BRDT-BD1, with IC₅₀s of 0.059, 0.127 and 0.245 μM, respectively ^[1].

HY-112149

ZL0420	Epigenetic Reader Domain	Inflammation/Immunology
ZL0420 is a potent and selective bromodomain-containing protein 4 (BRD4) inhibitor with IC₅₀ values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2.

HY-143328

PROTAC BRD4 Degrader-17	PROTACs Epigenetic Reader Domain Apoptosis	Cancer
PROTAC BRD4 Degrader-17 (compound 13i) is a potent PROTAC BRD4 Degrader, with IC₅₀ values of 29.54 nM (BRD4 *(BD1)) and 3.82 nM (BRD4* (BD2)). PROTAC BRD4 Degrader-17 significantly attenuates G2/M progression associated Cyclin B1 expression. PROTAC BRD4 Degrader-17 significantly induces apoptosis in MV-4-11 cells ^[1].

HY-112149A

(E/Z)-ZL0420	Epigenetic Reader Domain	Inflammation/Immunology Cancer
(E/Z)-ZL0420 is a racemic compound of (Z)-ZL0420 and (E)-ZL0420 isomers. (E)-ZL0420 is a potent and selective bromodomain-containing protein 4 (BRD4) inhibitor with IC₅₀ values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2 ^[1].

HY-131203

PROTAC BRD4 Degrader-6	PROTACs Epigenetic Reader Domain Apoptosis c-Myc Caspase	Cancer
PROTAC BRD4 Degrader-6 (compound 32a) is a potent small-molecule *BRD4*PROTAC degrader with IC₅₀ value of 2.7 nM for BRD4 BD1. PROTAC BRD4 Degrader-6 potently degrades BRD4 protein and inhibits the expression of c-Myc. PROTAC BRD4 Degrader-6 inhibits the proliferation of pancreatic cancer cell line BxPC3 and induces apoptosis. PROTAC BRD4 Degrader-6 can be used for human pancreatic cancer research (Pink: Mivebresib (HY-100015); Black: linker, Azido-PEG1-CH2CO2H (HY-108369); Blue: Lenalidomide (HY-A0003)) ^[1].

HY-143300

BRD4-BD1-IN-2	Epigenetic Reader Domain	Cardiovascular Disease Cancer
BRD4-BD1-IN-2 is a selective *BRD4-BD1* inhibitor, with an IC₅₀ of 2.51 µM (20-times greater than that of BD2). BRD4-BD1-IN-2 can be used in studies of cancer and cardiovascular diseases ^[1].

HY-142675

BRD4-BD1/2-IN-2	Epigenetic Reader Domain	Cancer
BRD4-BD1/2-IN-2 is a potent BRD4 BD2 inhibitor with IC₅₀s of <0.5 nM and <300 nM for BRD4 BD2 and BRD4 BD1, respectively (WO2021233371A1, compound 2) ^[1].

HY-146739

BRD4 Inhibitor-19	Epigenetic Reader Domain	Cancer
BRD4 Inhibitor-19 is a BET inhibitor with an IC₅₀ of 55 nM for BRD4-BD1. BRD4 Inhibitor-19 can be used for multiple myeloma research ^[1].

HY-111977

ZEN-3219	Epigenetic Reader Domain	Cancer
ZEN-3219 is a BET inhibitor with IC₅₀s of 0.48, 0.16 and 0.47 μM for *BRD4(BD1), BRD4(BD2)* and *BRD4(BD1BD2), respectively. ZEN-3219 can be used to form PROTACs to induce degradation of BRD4* ^[1].

HY-111979

ZEN-3411	Epigenetic Reader Domain	Cancer
ZEN-3411 is a BET inhibitor with IC₅₀s of 0.05, 0.05 and 0.06 μM for *BRD4(BD1), BRD4(BD2)* and *BRD4(BD1BD2), respectively. ZEN-3411 can be used to form PROTACs to induce degradation of BRD4* ^[1].

HY-111978

ZEN-3862	Epigenetic Reader Domain	Cancer
ZEN-3862 is a BET inhibitor with IC₅₀s of 0.16 and 0.13 μM for BRD4(BD1) and BRD4(BD2) , respectively. ZEN-3862 can be used to form PROTACs to induce degradation of BRD4 ^[1].

HY-173450

ZL0516	Epigenetic Reader Domain	Inflammation/Immunology
ZL0516 is a potent, selective, and orally active **BRD4 BD1 inhibitor. ZL0516 suppresses inflammatory bowel disease (IBD) by inhibiting BRD4/NF-κB** signaling ^[1].

HY-107425B

cis-MZ 1 hydrate	Epigenetic Reader Domain	Cancer
cis-MZ 1 hydrate is a negative control for *BRD4*-targeted PROTAC MZ 1 (HY-107425). cis-MZ 1 or MZ 1 is a combination of the von Hippel-Lindau ligand (red part in the structural formula) and the BRD4 ligand (blue part in the structural formula). The K_d of MZ 1 for BRD4 BD1/2 was 382 nM and 120 nM, respectively ^[1].

Cat. No.	Product Name		Classification

HY-136857

BRD4 degrader-3		PROTAC Synthesis
BRD4 degrader-3 is a potent bromodomain BRD4 degrader extracted from patent WO2020055976A1, example 1a, has IC₅₀s of 15.5 and 12.3 nM for BRD4-BD1 and BRD4-BD2, respectively ^[1]. PROTAC BRD4 Degrader-7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-133138

Pomalidomide-PEG1-azide		Azide PROTAC Synthesis
Pomalidomide-PEG1-azide is an E3 ligase lgand-linker conjugate. Pomalidomide-PEG1-azide incorporates the Pomalidomide based cereblon ligand and a linker. Pomalidomide-PEG1-azide can be used to synthesis PROTAC BRD4 Degrader-1 (HY-133131) ^[1]. PROTAC BRD4 Degrader-1 is a PROTAC connected by ligands for Cereblon and BRD4 with an IC₅₀ of 41.8 nM against **BRD4 BD1*. PROTAC BRD4* Degrader-1 can effectively degrade BRD4 protein and suppress c-Myc expression.

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BRD4 (BD1)

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